Division of Endocrinology, Central Drug Research Institute, Lucknow, India.
Reprod Toxicol. 2010 Apr;29(2):214-24. doi: 10.1016/j.reprotox.2009.11.001. Epub 2009 Nov 10.
Our interest in development of hyaluronidase inhibitors as male antifertility agents led to identification of Terminalia chebula (T. chebula) plant with hyaluronidase (HAase) inhibitory activity of human spermatozoa ( approximately 93% inhibition) and rat caudal epididymal spermatozoa ( approximately 86% inhibition) in vitro at 30 mg/ml. We further demonstrated inhibition of hyaluronidase activity of testis and epididymal spermatozoa in vivo coincident with antispermatogenic activity and contraceptive efficacy of TC extract administered at 50 and 100mg/kg/day orally for 60 days in male albino rats. The significant decrease in motility, count and increase in morphological abnormalities of epididymal spermatozoa and severe reduction in fertility (-100%) of male rats treated with T. chebula fruit extract at 100mg/kg dose could be attributed to either direct effect on testis or direct or indirect interference with sperm maturation in epididymis, and/or inhibition of testicular and epididymal sperm hyaluronidase enzyme in vivo probably caused by flavonoids like tannins present in T. chebula.
我们对透明质酸酶抑制剂作为男性抗生育剂的开发感兴趣，导致鉴定出Terminalia chebula（T. chebula）植物，其具有透明质酸酶（HAase）抑制活性，可在 30mg/ml 时体外抑制人精子（约 93%抑制）和大鼠尾附睾精子（约 86%抑制）。我们进一步证明，在雄性白化大鼠中，TC 提取物以 50 和 100mg/kg/天口服给药 60 天，可抑制睾丸和附睾精子的透明质酸酶活性，同时具有抗精子发生活性和避孕效果。在 100mg/kg 剂量下，T. chebula 果实提取物处理的附睾精子的运动性、计数和形态异常增加以及生育力严重降低（-100%），可能归因于对睾丸的直接影响，或直接或间接干扰附睾精子成熟，以及/或体内睾丸和附睾精子透明质酸酶的抑制，这可能是由于 T. chebula 中存在的类黄酮如单宁所致。
